Fragment splicing is a primary strategy in the design and optimization of leading compound toward new skeleton with target bioactivity. Herein a series of novel substituted phenyl oxazole derivatives were designed via fragment analysis and coupling strategy that led to highly potent and bio-selective herbicide safener. The biological tests showed that most of the compounds could enhance the maize growth
片段剪接是设计和优化领先化合物朝向具有目标
生物活性的新骨架的主要策略。在本文中,通过片段分析和偶联策略设计了一系列新颖的取代苯基
恶唑衍
生物,从而产生了高效且具有
生物选择性的
除草剂安全性。
生物学测试表明,大多数化合物在体内均可提高玉米生长指数,
谷胱甘肽含量和抗逆酶
谷胱甘肽S-转移酶活性。分子对接模型表明,该新化合物可与
氯磺隆竞争
除草剂目标酶的结合,从而实现
除草剂的解毒。尤其是化合物If表现出比商业上更安全的异恶二芬-乙基和其他化合物更好的活性。